Rizatriptan 5mg Tablets

Manufacturer AUROBINDO Active Ingredient Rizatriptan Tablets(rye za TRIP tan) Pronunciation rye za TRIP tan
It is used to treat migraine headaches.
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Drug Class
Antimigraine agent
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Pharmacologic Class
Selective serotonin (5-HT1B/1D) receptor agonist
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Pregnancy Category
C
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FDA Approved
Jun 1998
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Rizatriptan is a medication used to treat acute migraine headaches. It works by narrowing blood vessels in the brain and affecting certain nerves, which helps to relieve migraine pain and other symptoms like nausea and sensitivity to light and sound.
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How to Use This Medicine

Taking Your Medication Correctly

To get the most benefit from this medication, follow your doctor's instructions carefully. Read all the information provided to you and adhere to the guidelines below.

Administration Guidelines

You can take this medication with or without food.
It's best to take it as soon as possible after your headache starts.
Adults: If your headache doesn't improve after the first dose, consult your doctor. If your headache recurs, you may take a second dose only if your doctor has advised you to do so. Make sure to wait at least 2 hours after the first dose before taking the second dose.
Children: If your child's headache doesn't improve, improves but then returns, or if they only experience partial relief, consult your doctor before giving another dose.

Storage and Disposal

Store this medication at room temperature in a dry place, away from the bathroom.

Missed Dose

Since this medication is taken as needed, you don't need to worry about missing a dose. However, do not take it more frequently than prescribed by your doctor.
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Lifestyle & Tips

  • Take at the first sign of a migraine headache, but not for prevention.
  • Do not take more than 30 mg in 24 hours.
  • Avoid migraine triggers (e.g., certain foods, stress, lack of sleep).
  • Maintain a regular sleep schedule.
  • Stay hydrated.

Dosing & Administration

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Adult Dosing

Standard Dose: 5 mg or 10 mg orally, once. May repeat dose after 2 hours if migraine recurs. Max 30 mg in 24 hours.
Dose Range: 5 - 10 mg

Condition-Specific Dosing:

withPropranolol: Initial dose 5 mg, max 15 mg in 24 hours.
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Pediatric Dosing

Neonatal: Not established
Infant: Not established
Child: Not established
Adolescent: 6 to 17 years: 5 mg or 10 mg orally, once. Max 10 mg in 24 hours. (Note: Maxalt-MLT is approved for this age group, not standard tablets for all indications). For 6-11 years, 5 mg for body weight < 40 kg, 10 mg for body weight â‰Ĩ 40 kg. For 12-17 years, 10 mg.
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Dose Adjustments

Renal Impairment:

Mild: No adjustment needed
Moderate: No adjustment needed
Severe: Use with caution; limited data. Consider lower doses.
Dialysis: Not specifically studied; use with caution.

Hepatic Impairment:

Mild: No adjustment needed
Moderate: Initial dose 5 mg, max 15 mg in 24 hours.
Severe: Contraindicated due to increased plasma concentrations.

Pharmacology

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Mechanism of Action

Rizatriptan is a selective agonist for 5-hydroxytryptamine1B (5-HT1B) and 5-hydroxytryptamine1D (5-HT1D) receptors. Its therapeutic action in migraine is thought to be due to selective cranial vasoconstriction (via 5-HT1B receptors on intracranial blood vessels) and inhibition of neuropeptide release from trigeminal afferents (via 5-HT1D receptors on presynaptic nerve terminals). These actions lead to the attenuation of pain transmission in the trigeminal system.
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Pharmacokinetics

Absorption:

Bioavailability: Approximately 40-45%
Tmax: 1-1.5 hours (oral tablet); 1.6-2.5 hours (ODT)
FoodEffect: Food delays Tmax by approximately 1 hour but does not significantly affect bioavailability.

Distribution:

Vd: Approximately 110-140 L
ProteinBinding: Approximately 14%
CnssPenetration: Limited

Elimination:

HalfLife: 2-3 hours
Clearance: Approximately 1000 mL/min (renal clearance ~500 mL/min)
ExcretionRoute: Approximately 82% renal (17% unchanged drug, 65% metabolite), 12% fecal
Unchanged: Approximately 17%
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Pharmacodynamics

OnsetOfAction: Within 30 minutes to 2 hours
PeakEffect: 1-2 hours
DurationOfAction: Up to 24 hours (for migraine relief, though half-life is shorter)

Safety & Warnings

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Side Effects

Urgent Side Effects: Seek Medical Help Immediately

Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical attention right away:

Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of high blood pressure, including:
+ Severe headache or dizziness
+ Passing out
+ Changes in eyesight
Loss of eyesight, which can be long-lasting
Abnormal sensations, such as burning, numbness, or tingling
Severe stomach upset or vomiting
Severe stomach pain or bloody diarrhea
Feeling of heaviness or tightness in the leg muscles
Feeling cold
Serotonin syndrome, a potentially life-threatening condition, which may cause:
+ Agitation
+ Changes in balance
+ Confusion
+ Hallucinations
+ Fever
+ Fast or abnormal heartbeat
+ Flushing
+ Muscle twitching or stiffness
+ Seizures
+ Shivering or shaking
+ Excessive sweating
+ Severe diarrhea, stomach upset, or vomiting
+ Severe headache
Heart problems, including:
+ Heart attack
+ Abnormal heartbeat
+ Chest, throat, neck, or jaw tightness, pain, pressure, or heaviness
+ Cold sweats
+ Shortness of breath
+ Fast or abnormal heartbeat
+ Severe dizziness or passing out
Brain blood vessel problems, including:
+ Stroke
+ Weakness on one side of the body
+ Trouble speaking or thinking
+ Changes in balance
+ Drooping on one side of the face
+ Changes in eyesight

Other Possible Side Effects

Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to contact your doctor or seek medical help if you notice any of the following:

Feeling dizzy, sleepy, tired, or weak
Upset stomach
Other side effects that bother you or do not go away

Reporting Side Effects

If you have questions about side effects or want to report any, you can:

Contact your doctor for medical advice
Call the FDA at 1-800-332-1088
* Report side effects online at https://www.fda.gov/medwatch
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Seek Immediate Medical Attention If You Experience:

  • Sudden or severe chest pain, jaw pain, or arm pain (could be heart attack)
  • Shortness of breath
  • Weakness or numbness on one side of the body (could be stroke)
  • Vision changes
  • Severe stomach pain or bloody diarrhea (could be ischemic colitis)
  • Signs of serotonin syndrome: agitation, confusion, rapid heart rate, fever, sweating, muscle stiffness, twitching, loss of coordination, nausea, vomiting, diarrhea.
  • Allergic reactions: rash, hives, swelling of face/lips/tongue/throat, difficulty breathing.
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Before Using This Medicine

Before Taking This Medication: Important Information to Share with Your Doctor

It is essential to inform your doctor about the following conditions to ensure safe treatment:

Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Describe the allergic reaction and its symptoms.
If you have high blood pressure.
A history of certain health problems, including:
+ Chest pain or pressure
+ Diseased arteries in the legs or arms
+ Heart attack
+ Heart disease
+ Poor blood flow in the heart, brain, bowel, or kidney
+ Stroke or transient ischemic attack (TIA)
+ Certain types of migraines, such as hemiplegic or basilar migraines
+ Abnormal heartbeat, including Wolff-Parkinson-White syndrome
If you are taking propranolol.
If you have taken specific depression medications, such as isocarboxazid, phenelzine, or tranylcypromine, within the last 14 days. Taking this medication within 14 days of these drugs can cause severe high blood pressure.
If you have taken any of the following medications in the last 24 hours:
+ Almotriptan
+ Eletriptan
+ Frovatriptan
+ Naratriptan
+ Sumatriptan
+ Zolmitriptan
* If you have taken ergotamine, methysergide, dihydroergotamine, or similar medications in the last 24 hours.

This list is not exhaustive, and it is crucial to inform your doctor and pharmacist about all your medications, including prescription and over-the-counter drugs, natural products, and vitamins, as well as any health problems you have. Always check with your doctor before starting, stopping, or changing the dose of any medication to ensure your safety.
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Precautions & Cautions

It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. Until you understand how this drug affects you, avoid driving and other activities that require alertness.

Monitor your blood pressure as directed by your doctor, as this medication can cause high blood pressure. Regular blood pressure checks will help your doctor assess any potential changes.

This medication is not intended to prevent or reduce the frequency of migraine headaches. If you experience a headache that is different from your typical migraine, consult your doctor before taking this medication.

Be cautious not to exceed the prescribed dose or frequency, as taking more of this medication than directed can worsen your headaches.

If you have risk factors for heart disease, such as high blood pressure, high cholesterol, being overweight, having high blood sugar or diabetes, smoking, being a male over 40 years old, having a family history of early heart disease, or being a postmenopausal female, use this medication with caution and discuss your risks with your doctor.

If you are 65 years or older, use this medication with caution, as you may be more susceptible to side effects.

If you are pregnant, planning to become pregnant, or breastfeeding, inform your doctor to discuss the potential benefits and risks to you and your baby.
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Overdose Information

Overdose Symptoms:

  • Hypertension
  • Coronary vasospasm
  • Ischemic heart disease
  • Transient ischemic attacks
  • Stroke
  • Serotonin syndrome

What to Do:

Seek immediate medical attention. There is no specific antidote. General supportive measures should be employed. Monitor ECG and blood pressure. Call 1-800-222-1222 (Poison Control Center).

Drug Interactions

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Contraindicated Interactions

  • Monoamine Oxidase Inhibitors (MAOIs) or within 2 weeks of discontinuing MAOIs
  • Ergot-type drugs (e.g., ergotamine, dihydroergotamine, methysergide) or within 24 hours of using ergot-type drugs
  • Other 5-HT1 agonists (triptans) or within 24 hours of using other triptans
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Major Interactions

  • Propranolol (increases rizatriptan plasma levels; requires dose adjustment)
  • Selective Serotonin Reuptake Inhibitors (SSRIs) and Serotonin Norepinephrine Reuptake Inhibitors (SNRIs) (increased risk of serotonin syndrome)

Monitoring

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Baseline Monitoring

Cardiovascular risk assessment (e.g., blood pressure, ECG if indicated)

Rationale: To rule out underlying cardiovascular disease, as triptans can cause coronary vasospasm.

Timing: Prior to initiation, especially in patients with risk factors for CAD.

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Routine Monitoring

Migraine frequency and severity

Frequency: Each visit or as needed

Target: Reduction in migraine days/severity

Action Threshold: Lack of efficacy or worsening symptoms

Adverse effects (e.g., chest pain, neck tightness, paresthesias)

Frequency: Each visit or as needed

Target: Absence or tolerability of side effects

Action Threshold: Severe or persistent adverse effects

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Symptom Monitoring

  • Chest pain or tightness (could indicate cardiac ischemia)
  • Shortness of breath
  • Numbness or tingling
  • Weakness or heaviness in limbs
  • Signs of serotonin syndrome (agitation, hallucinations, rapid heart beat, fever, overactive reflexes, nausea, vomiting, diarrhea, incoordination)
  • Signs of allergic reaction (rash, hives, swelling of face/lips/tongue/throat, difficulty breathing)

Special Patient Groups

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Pregnancy

Rizatriptan is Pregnancy Category C. Use only if the potential benefit justifies the potential risk to the fetus. Limited human data suggest no increased risk of major birth defects, but animal studies show some adverse effects at high doses.

Trimester-Specific Risks:

First Trimester: Limited human data, no clear increased risk of major birth defects identified.
Second Trimester: Limited human data, no clear increased risk.
Third Trimester: Limited human data, no clear increased risk. Theoretical risk of uterine contractions or fetal vascular effects, but not well-established.
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Lactation

Rizatriptan is excreted into breast milk. The amount is small, and the relative infant dose is low. The American Academy of Pediatrics considers triptans compatible with breastfeeding. Monitor infant for drowsiness or poor feeding.

Infant Risk: Low risk (L3). Consider waiting 12-24 hours after a dose before breastfeeding to minimize infant exposure, though this may not be necessary for all infants.
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Pediatric Use

Approved for acute treatment of migraine with or without aura in adolescents 6 to 17 years of age (Maxalt-MLT). Dosing is weight-based for younger children. Safety and efficacy not established for children under 6 years.

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Geriatric Use

Use with caution in elderly patients (over 65 years) due to a higher likelihood of underlying cardiovascular disease and potential for increased sensitivity to adverse effects. No specific dose adjustment is generally required unless hepatic or renal impairment is present.

Clinical Information

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Clinical Pearls

  • Rizatriptan is effective for acute migraine treatment, but not for prevention.
  • It is available as a standard tablet and an orally disintegrating tablet (Maxalt-MLT), which can be beneficial for patients with nausea or difficulty swallowing.
  • Instruct patients to take the medication as soon as migraine symptoms begin, but not before the onset of headache.
  • Counsel patients on the importance of not exceeding the maximum daily dose and the 2-hour interval between doses.
  • Always screen patients for cardiovascular risk factors before prescribing triptans.
  • Warn patients about the risk of serotonin syndrome when co-administered with SSRIs or SNRIs.
  • Patients should be advised to seek immediate medical attention for any signs of serious adverse events like chest pain or neurological symptoms.
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Alternative Therapies

  • Other triptans (e.g., sumatriptan, zolmitriptan, eletriptan, frovatriptan, naratriptan, almotriptan)
  • NSAIDs (e.g., ibuprofen, naproxen)
  • Acetaminophen
  • Ergot alkaloids (e.g., ergotamine, dihydroergotamine)
  • CGRP receptor antagonists (e.g., rimegepant, ubrogepant)
  • Ditans (e.g., lasmiditan)
  • Anti-emetics (e.g., metoclopramide, prochlorperazine) for associated nausea/vomiting
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Cost & Coverage

Average Cost: Varies widely, typically $10-$50 per 30 tablets
Generic Available: Yes
Insurance Coverage: Tier 1 or 2 (generic), Tier 3 (brand)
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General Drug Facts

If your symptoms or health issues persist or worsen, it's essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so be sure to check with your pharmacist for more information. If you have any questions or concerns about this medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When seeking help, be prepared to provide details about the overdose, including the medication taken, the amount, and the time it occurred.